1. Signaling Pathways
  2. Protein Tyrosine Kinase/RTK
  3. VEGFR

VEGFR

Vascular endothelial growth factor receptor

VEGFRs consist of three subtypes, the fms-like tyrosine kinase Flt-1 (VEGFR1/Flt-1), the kinase domain region, also referred to as fetal liver kinase (VEGFR2/KDR/Flk-1), and Flt-4 (VEGFR3). Each receptor has seven immunoglobulinlike domains in the extracellular domain, a single transmembrane region, and a consensus tyrosine kinase sequence interrupted by a kinase insert domain. VEGFR1 and 2 are expressed on vascular endothelial cells, whereas VEGFR3 is expressed on lymphatic endothelial. The VEGF family members VEGF-A, -B, -C, -D, -E, and PlGF, and the human immunodeficiency (HIV) Tat protein bind in specific patterns to three related receptor protein tyrosine kinases, VEGFR1, 2, and 3, and induce the formation of homo- and heteromeric receptor complexes. Binding of VEGF to VEGFR causes dimerization and autophosphorylation of the receptor. Intracellular proteins such as VEGFR-associated protein (VRAP), PLC, and Sck that associate with specific tyrosine residues of VEGFR are phosphorylated upon receptor activation. Several signal transduction pathways are activated by the binding of VEGF to its receptor, leading to increased proliferation, survival, permeability, and migration of cells.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-P99576
    Tarcocimab
    Inhibitor 98.35%
    Tarcocimab (OG1953) is a humanized anti-VEGFA monoclonal antibody (IgG1 type). Tarcocimab is available for research in retinal vein occlusion (RVO) and wet age-related macular degeneration (AMD).
    Tarcocimab
  • HY-12018A
    Vatalanib hydrochloride
    Inhibitor
    Vatalanib (PTK787; ZK-222584; CGP-797870) hydrochloride is an inhibitor of VEGFR2/KDR with an IC50 of 37 nM.
    Vatalanib hydrochloride
  • HY-50751G
    Linifanib (GMP)
    Inhibitor
    Linifanib (ABT-869) (GMP) is Linifanib (HY-50751) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Linifanib is a potent and orally active multi-target inhibitor of VEGFR and PDGFR family with IC50s of 4, 3, 66, and 4 nM for KDR, FLT1, PDGFRβ, and FLT3, respectively. Linifanib (GMP) promotes the generation and reprogramming of iPSCs from somatic cells.
    Linifanib (GMP)
  • HY-10407G
    SU 5402 (GMP)
    Inhibitor
    SU 5402 (GMP) is SU 5402 (HY-10407) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. SU 5402 is a potent multi-targeted receptor tyrosine kinase inhibitor with IC50 of 20 nM, 30 nM, and 510 nM for VEGFR2, FGFR1, and PDGFRβ, respectively.
    SU 5402 (GMP)
  • HY-P990961
    Palverafusp alfa
    Inhibitor
    Palverafusp alfa is an VEGFA/PDCD1-targeting IgG1κ type humanized antibody, the recommed isotype control is Human IgG1 kappa, Isotype Control (HY-P99001).
    Palverafusp alfa
  • HY-N0545R
    Taurocholic acid (sodium) (Standard)
    Agonist
    Taurocholic acid (sodium) (Standard) is the analytical standard of Taurocholic acid (sodium). This product is intended for research and analytical applications. Taurocholic acid sodium (Sodium taurocholate) has marked bioactive effects such as an inhibitory potential against hepatic artery ligation induced biliary damage by upregulation of VEGF-A expression. Taurocholic acid sodium has immunoregulation effect.
    Taurocholic acid (sodium) (Standard)
  • HY-18185
    JNJ 17029259
    Inhibitor
    JNJ 17029259 is an orally active and selective VEGF-R2 kinase inhibitor. JNJ 17029259 inhibits VEGF-mediated signal transduction. JNJ 17029259 has anti-angiogenic activity.
    JNJ 17029259
  • HY-147800
    VEGFR-2-IN-21
    Inhibitor
    VEGFR-2-IN-21 (Compound 5d) is a potent VEGFR-2 inhibitor with an IC50 of 0.10 μM. VEGFR-2-IN-21 shows anticancer activity.
    VEGFR-2-IN-21
  • HY-169100
    Antiproliferative agent-57
    Inhibitor
    Antiproliferative agent-57 (compound M2) is a tumor angiogenesis inhibitor. Antiproliferative agent-57 inhibits the secretion of VEGF in SiHa cells under hypoxic conditions (IC50=0.68 μM) without inducing cytotoxicity. Antiproliferative agent-57 can modulate the PI3K/AKT/mTOR and MAPK signaling pathways in tumor cells to inhibit the expression of HIF-1α and VEGF in tumor tissues.
    Antiproliferative agent-57
  • HY-155239
    VEGFR-2-IN-35
    Inhibitor
    VEGFR-2-IN-35 (compound 7) is a potent VEGFR-2 inhibitor with IC50=37 nM. VEGFR-2-IN-35 inhibits MCF-7 and HCT 116 cancer cells with IC50 values of 10.56 and 7.07 μM, respectively.
    VEGFR-2-IN-35
  • HY-101990
    IMS2186
    Inhibitor 99.81%
    IMS2186 is an anti-choroidal neovascularization (CNV) agent that inhibits angiogenesis upstream of VEGF. IMS2186 can arrest cancer cell cycle in G2/M phase, thus exerting anti-proliferation and anti-angiogenesis effects. IMS2186 has no intraocular toxicity and reduces the amount of eye leakage and diseased cells.
    IMS2186
  • HY-161586
    Chloramphenicol/BSA
    Inhibitor
    Chloramphenicol/BSA is the antigen-adjuvant conjugate formed by the coupling of Chloramphenicol (HY-B0239) with Bovine Serum Albumin (BSA). By conjugating the antigen with a protein adjuvant, the production of antigen-specific antibodies in vaccine models can be enhanced. The conjugate does not affect protein folding or disrupt major epitopes, and it can enhance cross-presentation and the generation of antigen-specific T cells.
    Chloramphenicol/BSA
  • HY-164413
    CLM3
    Inhibitor
    CLM3, a pyrazolopyrimidine derivative, is a multiple tyrosine kinase inhibitor. CLM3 shows antiproliferative and proapoptotic activity on endothelial and cancer cells, synergistically enhanced by SN38 (HY-13704). These effects are mainly due to its inhibition of phosphorylation of VEGFR-2, EGFR and RET tyrosine kinases and their related signaling pathways.
    CLM3
  • HY-157324
    EGFR-IN-94
    Inhibitor
    EGFR-IN-94 (compound 5a) is a EGFR inhibitor with IC50 of 0.086?μM, and also has IC50 of 0.107μM and 2.52 μM for VEGFR-2 and Topo II, respectively. EGFR-IN-94 induces cell apoptosis and arrests cell cycle at the S phase in HepG-2 cells .
    EGFR-IN-94
  • HY-168114
    Multi-kinase inhibitor 3
    Inhibitor
    Multi-kinase inhibitor 3 (compound 12) is a potent and orally active multikinase inhibitor with IC50 values of 1.59, 1.23, 1.19, 0.59, 0.22, 1.15 nM for FLT1/VEGFR1, KDR/VEGFR2, FLT4/VEGFR3, FLT3, PDGFRα, PDGFRβ, respectively. Multi-kinase inhibitor 3 shows antiproliferative activity. Multi-kinase inhibitor 3 shows anticancer activity.
    Multi-kinase inhibitor 3
  • HY-155760
    hCA/VEGFR-2-IN-3
    Inhibitor
    hCA/VEGFR-2-IN-3 (compound 8j) is an indolinonylbenzenesulfonamide and a potential dual inhibitor of cancer-associated hCA IX/XII and VEGFR-2. hCA/VEGFR-2-IN-3 inhibits VEGFR-2 (IC50=358 nM), has high binding activity to hCAs with Ki of 4.2 nM (hCA IX), 22.9 nM (hCA II), 25.1 nM (hCA I), 28.0 nM (hCA XII), respectively. hCA/VEGFR-2-IN-3 has antiproliferative activity against VEGFR-2 overexpressing breast cancer cells.
    hCA/VEGFR-2-IN-3
  • HY-P990318
    Alacizumab
    Inhibitor
    Alacizumab is a CHO-expressed humanized antibody that targets VEGFR2/KDR/CD309. Alacizumab contains huIgG1 heavy chain and huκ light chain, with a predicted molecular weight (MW) of 144.08 kDa. The isotype control for Alacizumab can be referenced as Human IgG1 kappa, Isotype Control (HY-P99001).
    Alacizumab
  • HY-10981S1
    Lenvatinib-d5
    Inhibitor
    Lenvatinib-d5 is the deuterium labeled Lenvatinib. Lenvatinib (E7080) is an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities[1][2].
    Lenvatinib-d<sub>5</sub>
  • HY-P10833
    C-VGB3
    Antagonist
    C-VGB3 is a selective vascular endothelial growth factor receptor 2 (VEGFR2) antagonist, which inhibits VEGFR2-mediated PI3K/AKT/mTOR and PLCγ/ERK1/2 signaling pathways. C-VGB3 binds to the extracellular domain of VEGFR2, blocking ligand-receptor interaction and inducing apoptosis in endothelial and tumor cells through both intrinsic (involving Bcl2 family and caspases) and extrinsic (death receptor-mediated) pathways. C-VGB3 is promising for research of angiogenesis-related cancers, such as breast cancer.
    C-VGB3
  • HY-158233
    Apoptotic agent-4
    Inhibitor
    Apoptotic agent-4 (Compound 9) is a apoptosis inducer. Apoptotic agent-4 inhibits VEGFR-2 with an IC50 of 0.5717 μM. Apoptotic agent-4 inhibits cancer cell proliferation and arrests the cell at both the G2/M and Pre-G1 phases.
    Apoptotic agent-4
Cat. No. Product Name / Synonyms Species Source
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